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Assay Detail

CHEMBL640473

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Binding
Displacement of [3H]CHA from Adenosine A1 receptor of rat brain
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-alkenyl and 2-alkyl derivatives of adenosine and adenosine-5'-N-ethyluronamide: different affinity and selectivity of E- and Z-diastereomers at A2A adenosine receptors.
Vittori S, Camaioni E, Di Francesco E, Volpini R, Monopoli A, Dionisotti S, Ongini E, Cristalli G.
J Med Chem (1996) 39 : 4211 -4217
PubMed 8863798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.63 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.98
CHEMBL319387 1 7.01
CHEMBL2113526 1 6.93
CHEMBL410873 1 6.89
CHEMBL2113450 1 6.68
CHEMBL2113528 1 6.60
CHEMBL98603 1 6.48
CHEMBL2113527 1 6.21
CHEMBL223270 1 6.16
CHEMBL611256 1 6.02
CHEMBL2304158 1 5.99
CHEMBL2113529 1 -
CHEMBL608918 1 -
CHEMBL2113525 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 10.4 nM 7.98
CHEMBL319387 Ki = 98.0 nM 7.01
CHEMBL2113526 Ki = 117.0 nM 6.93
CHEMBL410873 Ki = 130.0 nM 6.89
CHEMBL2113450 Ki = 209.0 nM 6.68
CHEMBL2113528 Ki = 251.0 nM 6.60
CHEMBL98603 Ki = 332.0 nM 6.48
CHEMBL2113527 Ki = 618.0 nM 6.21
CHEMBL223270 Ki = 698.0 nM 6.16
CHEMBL611256 Ki = 951.0 nM 6.02
CHEMBL2304158 Ki = 1017.0 nM 5.99
CHEMBL2113529 Ki > 1.0 nM -
CHEMBL608918 Ki > 1.0 nM -
CHEMBL2113525 Ki > 1.0 nM -